Triggered drug release from an antibody-drug conjugate using fast "click-to-release" chemistry in mice

Raffaella Rossin; Sander M.J. van Duijnhoven; Wolter Ten Hoeve; Henk M. Janssen; Laurens H.J. Kleijn; Freek J.M. Hoeben; Ron M. Versteegen; Marc S. Robillard

doi:10.1021/acs.bioconjchem.6b00231

Triggered drug release from an antibody-drug conjugate using fast "click-to-release" chemistry in mice

Raffaella Rossin, Sander M.J. van Duijnhoven, Wolter Ten Hoeve, Henk M. Janssen, Laurens H.J. Kleijn, Freek J.M. Hoeben, Ron M. Versteegen, Marc S. Robillard (Corresponding author)

Onderzoeksoutput: Bijdrage aan tijdschrift › Tijdschriftartikel › Academic › peer review

100 Citaten (Scopus)

Samenvatting

The use of a bioorthogonal reaction for the selective cleavage of tumor-bound antibody-drug conjugates (ADCs) would represent a powerful new tool for ADC therapy, as it would not rely on the currently used intracellular biological activation mechanisms, thereby expanding the scope to noninternalizing cancer targets. Here we report that the recently developed inverse-electron-demand Diels-Alder pyridazine elimination reaction can provoke rapid and self-immolative release of doxorubicin from an ADC in vitro and in tumor-bearing mice.

Originele taal-2	Engels
Pagina's (van-tot)	1697-1706
Aantal pagina's	10
Tijdschrift	Bioconjugate Chemistry
Volume	27
Nummer van het tijdschrift	7
DOI's	https://doi.org/10.1021/acs.bioconjchem.6b00231
Status	Gepubliceerd - 20 jul 2016

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10.1021/acs.bioconjchem.6b00231

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Citeer dit

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author = "Raffaella Rossin and {van Duijnhoven}, {Sander M.J.} and {Ten Hoeve}, Wolter and Janssen, {Henk M.} and Kleijn, {Laurens H.J.} and Hoeben, {Freek J.M.} and Versteegen, {Ron M.} and Robillard, {Marc S.}",

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Triggered drug release from an antibody-drug conjugate using fast "click-to-release" chemistry in mice. / Rossin, Raffaella; van Duijnhoven, Sander M.J.; Ten Hoeve, Wolter; Janssen, Henk M.; Kleijn, Laurens H.J.; Hoeben, Freek J.M.; Versteegen, Ron M.; Robillard, Marc S. (Corresponding author).

In: Bioconjugate Chemistry, Vol. 27, Nr. 7, 20.07.2016, blz. 1697-1706.

Onderzoeksoutput: Bijdrage aan tijdschrift › Tijdschriftartikel › Academic › peer review

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